Antibacterial resistance is a global clinical and public health problem that has emerged with alarming rapidity in recent years and undoubtedly will increase in the near future. Resistance is a problem in the community as well as in health care settings, where transmission of bacteria is greatly amplified. Because multiple drug resistance is a growing problem, physicians are now confronted with infections for which there is no effective therapy. The morbidity, mortality, and financial costs of such infections pose an increasing burden for health care systems worldwide. Strategies to address these issues emphasize enhanced surveillance of drug resistance, increased monitoring and improved usage of antimicrobial drugs, professional and public education, development of new drugs, and assessment of alternative therapeutic modalities.
As a result, alternative and improved agents are needed for the treatment of bacterial infections, particularly for the treatment of infections caused by resistant strains of bacteria, e.g., penicillin-resistant, methicillin-resistant, ciprofloxacin-resistant, and/or vancomycin-resistant strains.
WO2004/031195, published Apr. 15, 2004, discloses tricyclic tetrahydroquinoline antibacterial agents.
WO2007/072151, published Jun. 28, 2007, discloses 8-pyrazinyl-S-spiropyrimidinetrione-oxazinoquinoline derivatives as antibacterial agents.
WO2009/004382, published Jan. 8, 2009, discloses 3-spiropyrimidinetrione-quinoline derivatives and their use as antibacterial agents.
WO2006/120563, published Nov. 16, 2006, discloses thiadiazol-spiropyrimidinetrione-quinoline derivatives and their use as antibacterial agents.
Brian S. Gerstenberger, Mark R. Rauckhorst and Jeremy T. Starr, “One-Pot Synthesis of N-Arylpyrazoles from Arylhalides,” Organic Letters, 2009, Vol. 11, Nol. 10, 2097-2100, discloses a one-pot method for the synthesis of diversely functionalized pyrazoles.